Vps34-IN-5 

Vps34-IN-5 is an orally active VPS34 inhibitor, 98% target inhibition, and an IC₅₀ categorized as B. Vps34-IN-5 induces additive or synergistic anti-proliferative activity with EGFR inhibitors in cancer cells. Vps34-IN-5 is administered orally alone or with Erlotinib (HY-50896) in mouse xenograft models. Vps34-IN-5 can be used for the research of non-small cell lung cancer^[1].

Vps34-IN-5 (Ⅰ-299) exhibits additive anti-proliferative activity in combination with Erlotinib (HY-50896), Afatinib (HY-10261), AZD9291 (HY-15772), or CO-1686 (HY-15729) in A431 cells, with combination indices ranging from 1.00 to 1.02^[1].
Vps34-IN-5 exhibits synergistic anti-proliferative activity in combination with afatinib, CO-1686, or erlotinib, and additive activity with AZD9291, in NCI H-1650 cells^[1].
Vps34-IN-5 exhibits synergistic anti-proliferative activity in combination with afatinib or AZD9291, and additive activity with CO-1686, in NCI-H1975 cells^[1].
Vps34-IN-5 exhibits additive anti-proliferative activity in combination with erlotinib, AZD9291, or CO-1686, and subadditive activity with afatinib, in PC9 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Vps34-IN-5 (0.65 mg/kg; p.o.; daily; 21 days) inhibits tumor growth when used alone in nude female mice bearing human tumor xenografts^[1].
Vps34-IN-5 (0.65 mg/kg; p.o.; daily; 21 days) plus erlotinib (50/mg/kg) reduces tumor volume when used alone in nude female mice bearing human tumor xenografts^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

502.92

C₂₂H₁₇ClF₂N₆O₂S

1801903-15-0

O=S(NC1=C(N=CC(C2=CC(NC3=NC(C)=NC=C3)=NC=C2)=C1C)Cl)(C4=CC=C(C=C4F)F)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Bharathan IT, et al. Heteroaryls and uses thereof. United State, WO2015108861 A. 2015-07-23.